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100mg |
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250mg |
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500mg |
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2g |
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5g |
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Purity: ≥98%
Gemcitabine HCl (formerly also known as LY-188011, NSC-613327; dFdC; dFdCyd; trade name: Gemzar), the hydrochloride salt of gemcitabine which is an antimetabolite anticancer drug, is a potent DNA synthesis inhibitor approved for cancer treatment. In PANC1, MIAPaCa2, BxPC3, and Capan2 cells, it inhibits DNA synthesis with IC50s of 50 nM, 40 nM, 18 nM, and 12 nM, respectively. Difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP) are the active metabolites of gemcitabine that are produced intracellularly. The deoxynucleotide pool available for DNA synthesis is reduced when dFdCDP inhibits ribonucleotide reductase.
Targets |
DNA synthesis (Capan2 cells) ( IC50 = 12 nM ); DNA synthesis (BxPC3 cells) ( IC50 = 18 nM ); DNA synthesis (MIAPaCa2 cells) ( IC50 = 40 nM ); DNA synthesis (PANC1 cells) ( IC50 = 50 nM )
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ln Vitro |
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ln Vivo |
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Cell Assay |
In a 96-well plate, BxPC-3, MIA PaCa-2, and PANC-1 cells are seeded. Cells are treated for a further 24 or 48 hours with vehicle, DMAPT, and/or Gemcitabine after 24 hours. Using the Cell Death Detection ELISA, apoptosis is measured in relation to vehicle-treated cells by counting the quantity of cytoplasmic histone-associated DNA fragments.
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Animal Protocol |
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References |
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Molecular Formula |
C9H11F2N3O4.HCI
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Molecular Weight |
299.66
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Exact Mass |
299.05
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Elemental Analysis |
C, 36.07; H, 4.04; Cl, 11.83; F, 12.68; N, 14.02; O, 21.36
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CAS # |
122111-03-9
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Appearance |
White solid powder
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SMILES |
C1=CN(C(=O)N=C1N)[C@H]2C([C@@H]([C@H](O2)CO)O)(F)F.Cl
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InChi Key |
OKKDEIYWILRZIA-OSZBKLCCSA-N
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InChi Code |
InChI=1S/C9H11F2N3O4.ClH/c10-9(11)6(16)4(3-15)18-7(9)14-2-1-5(12)13-8(14)17;/h1-2,4,6-7,15-16H,3H2,(H2,12,13,17);1H/t4-,6-,7-;/m1./s1
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Chemical Name |
4-amino-1-[(2R,4R,5R)-3,3-difluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one;hydrochloride
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Synonyms |
Abbreviations: dFdC; dFdCyd; LY188011; LY-188011; LY 188011; gemcitabine; Gemzar
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3371 mL | 16.6856 mL | 33.3712 mL | |
5 mM | 0.6674 mL | 3.3371 mL | 6.6742 mL | |
10 mM | 0.3337 mL | 1.6686 mL | 3.3371 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02769832 | Active Recruiting |
Drug: Nab-paclitaxel Drug: Gemcitabine |
Small Cell Lung Cancer (SCLC) |
Muhammad Furqan | August 29, 2016 | Phase 2 |
NCT00479128 | Active Recruiting |
Drug: Bortezomib Drug: Gemcitabine |
Solid Tumor Urethral Cancer |
M.D. Anderson Cancer Center | September 28, 2006 | Phase 1 |
NCT03520790 | Active Recruiting |
Drug: Gemcitabine Other: Placebo |
Pancreatic Cancer | Dana-Farber Cancer Institute | December 5, 2018 | Phase 1 Phase 2 |
NCT03558087 | Active Recruiting |
Drug: Nivolumab Drug: Gemcitabine |
Bladder Cancer | Matthew Galsky | July 13, 2018 | Phase 2 |
NCT03507491 | Active Recruiting |
Drug: Gemcitabine Drug: Nab-paclitaxel |
Cancer | Emory University | August 27, 2018 | Phase 1 |
Cytotoxicity of I3C and gemcitabine (GEM) at clinical relevant concentrations in hTERT-HPNE and BxPC-3 cells cells. Anticancer Res . 2011 Oct;31(10):3171-80. td> |
Effect of I3C in combination with gemcitabine (GEM) on hENT1 protein expression in pancreatic cancer cell lines. Anticancer Res . 2011 Oct;31(10):3171-80. td> |
Combined inhibition of hTrx1 and RRM1 produced a synergistic anticancer effect in cancer cells and xenograft mice. A, SW480 or SW620 cells were treated with the indicated concentrations of gemcitabine or PX-12 for 72 h, and cell viability was measured with Cell Counting Kit-8 assays. J Biol Chem . 2017 Jun 2;292(22):9136-9149. td> |